SGC-GAK-1

产品编号: DC12565 Featured
SGC-GAK-1
结构式
2226517-76-4
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中国地区超过5000个高品质化合物库存
应用领域
SGC-GAK-1 是一种有效的选择性细胞周期蛋白 G 相关激酶 (GAK) 抑制剂,Ki 为 3.1 nM。SGC-GAK-1 是 GAK 的化学探针。
Cas No.: 2226517-76-4
名称: 6-bromo-N-(3,4,5-trimethoxyphenyl)quinolin-4-amine
别名: GAK inhibitor 1
SMILES: N1C2C(=CC(Br)=CC=2)C(NC2=CC(OC)=C(OC)C(OC)=C2)=CC=1
分子式: C18H17BrN2O3
分子量: 389.249
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: SGC-GAK-1 (GAK inhibitor 1) is a potent, selective, and cell-active inhibitor of cyclin G-associated kinase (GAK) with Ki of 3.2 nM, 16,000-fold selectivity over NAK; SGC-GAK-1 is highly selective in an in vitro kinome-wide screen, but cellular engagement assays defined RIPK2 as a collateral target; shows high affinity for GAK in cells in cellular target engagement assays (IC50=120 nM), 3-fold selectivity over RIPK2 in cells (IC50=360 nM); robustly blocked growth of 22Rv1 and LNCaP cell lines (Viability IC50=0.17 and 0.65 uM) that express AR splice variants associated with poor clinical prognosis, treatment of 22Rv1 cells with led to PARP cleavage, a marker of cells undergoing apoptosis, and an increase in phosphorylated histone H3 Ser10, as had been observed in with GAK targeting siRNA.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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